Lacosamide, also known as 2(R)-acetamido-N-benzyl-3-methoxypropionamide, acts as an NMDA glycine-site antagonist with a dual mode of action: selectively enhancing sodium channel inactivation and modulating collapsin response mediator protein-2. (Doty, P et al, Neurotherapeutics, 2007, 4(1): 145).
Lacosamide is currently in clinical trials for epilepsy, migraine, diabetic neuropathy, fibromyalgia, and osteoarthritis.
Lacosamide is converted, in vitro, to inactive metabolites, 30% of which is the O-demethylated product. (Bialer, M et al, Epilepsy Research, 2002, 51: 31-71).
The most frequently reported adverse events among patients dosed with lacosamide include headache, dizziness, fatigue, oral paraesthesia, diplopia and nausea—generally of short duration and mild in intensity (Sachdeo, R C et al, Neurology, 2003, 60 (5, suppl. 1): Abst S54.007).
Despite the beneficial activities of lacosamide, there is a continuing need for new compounds to treat the aforementioned diseases and conditions.